Method for preparing low dose pharmaceutical products

Abstract

A process for making pharmaceutical dosage units containing a therapeutic quantity of one or more low dosage medicinal agent comprising granulating said medicinal agent in an aqueous medium which contains a pharmaceutically acceptable surfactant agent and, optionally, further processing the product of said granulating into a tablet or capsule dosage unit.

What is claimed is: 
     
       1. A process for making pharmaceutical dosage units containing a therapeutic quantity of one or more low dosage medicinal agents comprising the steps of; (a) preparing an aqueous medium comprising one or more pharmaceutically acceptable surfactants, wherein the quantity of said surfactant or surfactants is sufficient to support said medical agent in solution; and   (b) granulating said one or more low dosage medicinal agents in said aqueous medium to form a granulation.   
     
     
       2. The process of claim 1 wherein one or more low dosage medicinal agent has a steroidal structure. 
     
     
       3. The process of claim 2 wherein said medicinal agent is an estrogen and, optionally, a progestin. 
     
     
       4. The process of claim 3 wherein said estrogen is estradiol or esterified estrogens. 
     
     
       5. The process of any one of claims 1, 2, 3, and 4 wherein the aqueous medium is water and said surfactant is sodium lauryl sulfate. 
     
     
       6. The process of claim 5 wherein the product form made by said process is a tablet. 
     
     
       7. A pharmaceutical composition made by the process as claimed in any one of claims 1, 2, 3, 4, 18, 21, 22, 25, or 26. 
     
     
       8. A pharmaceutical composition as claimed in claim 7 wherein the aqueous medium is water and the surfactant is sodium lauryl sulfate. 
     
     
       9. A pharmaceutical composition comprising a therapeutic quantity of one or more low dosage medicinal agent and one or more pharmaceutically acceptable surfactant in an aqueous medium and, optionally, one or more manufacturing additives and binding-granulating agents. 
     
     
       10. The composition of claim 9 wherein said one or more low dosage medicinal agent has a steroidal structure. 
     
     
       11. The composition of claim 10 wherein said medicinal agent is an estrogen and, optionally, a progestin. 
     
     
       12. The composition of claim 11 wherein said estrogen is estradiol or esterified estrogens. 
     
     
       13. The composition of any one of claims 9 to 12 wherein the aqueous medium is water, water from a povidone solution, or water and a water-miscible solvent. 
     
     
       14. The composition of claim 13 wherein said composition is in the form of a tablet, lozenge, troche, or capsule. 
     
     
       15. The composition of claim 14 wherein said composition is in the form of a tablet. 
     
     
       16. The composition of claim 13 wherein said surfactant is sodium lauryl sulfate. 
     
     
       17. The composition of claim 15 wherein said surfactant is sodium lauryl sulfate. 
     
     
       18. A method for evenly distributing the active ingredient of a low dosage medicinal agent in a pharmaceutically acceptable carrier comprising: (a) preparing an aqueous medium comprising one or more pharmaceutically acceptable surfactants, wherein the quantity of said surfactant or surfactants is sufficient to support said medicinal agent in solution; and   (b) granulating said active ingredient in said aqueous medium to form a granulation.   
     
     
       19. A method of claim 18 wherein said medicinal agent is an estrogen and, optionally, a progestin. 
     
     
       20. A method of claim 19 wherein said medicinal agent is estradiol. 
     
     
       21. The process of claim 1, wherein said quantity of said one or more pharmaceutically acceptable surfactants is less than 0.01% by weight of said granulation. 
     
     
       22. The process of claim 21,wherein the quantity of said one or more pharmaceutically acceptable surfactant is not more than 0.005% by weight of said granulation. 
     
     
       23. The composition of claim 9 wherein said quantity of said one or more pharmaceutically acceptable surfactants is less than 0.01% by weight of the composition. 
     
     
       24. The composition of claim 23 wherein the quantity of said one or more pharmaceutically acceptable surfactant is not more than 0.005% by weight of the composition. 
     
     
       25. The process of claim 1, further comprising the step of processing said granulation into a tablet or capsule dosage unit. 
     
     
       26. The process of claim 18, further comprising the step of processing said granulation into a tablet or capsule dosage unit.